Kontakt 2007, 9(2):403-406 | DOI: 10.32725/kont.2007.061

Epothilones - new anti-cancer medicinesBiomedicine

Jiří Patočka^*, Zdeněk Hon

Jihočeská univerzita v Českých Budějovicích, Zdravotně sociální fakulta, katedra radiologie a toxikologie

Epothilones are a new group of cytotoxic molecules, originally identified as metabolites produced by the myxobacterium Sorangium cellulosum. Clinical success of paclitaxel and docetaxel stimulated the research of further substances with the same mechanism of effects and resulted in discovering three new types of natural substances of non-taxane type: Epothilones A and B from a soil bacterium, discodermolide from a sponge and eleutherobines and sarcodictyines from corals. All the three groups of substances stabilize microtubules and competitively inhibit the bond of paclitaxel to polymers of tubulin, which suggests that their binding sites are the same. Epothilones are natural substances stabilizing microtubules with strong in vivo and in vitro anti-cancer activity. Thus, epothilones were considered as potential chemotherapeutic drugs due to their intervention into the cytoskeleton. Recent studies in cancer cell lines and in humans with cancer diseases indicate their higher efficacy compared with taxanes. The mechanism of their effects is similar to that of taxanes, but their chemical structure is simpler and their solubility in water is higher. In addition, epothilones may be prepared in large amounts by the fermentation of bacteria and they also exert activities against cell lines and tumours, which are resistant to many other drugs. Due to their high activity and to clinical requirements for the treatment of cancer, epothilones are targets of many studies. The purpose of the present article is to familiarize Czech readers with problems of epothilones.

Keywords: Chemotherapeutic drug; inhibitor of microtubules; Myxobacteria; review

Received: September 3, 2007; Accepted: October 15, 2007; Published: December 21, 2007  Show citation